title: 2,3-Substituted quinoxalin-6-amine analogs as antiproliferatives: a structure-activity relationship study.
abstract: The quinoxaline core is considered a privileged scaffold as it is found in a variety of biologically relevant molecules. Here we report the synthesis of a quinoxalin-6-amine library, screening against a panel of cancer cell lines and a structure-activity relationship (SAR). This resulted in the identification of a bisfuranylquinoxalineurea analog (7c) that has low micromolar potency against the panel of cancer cell lines. We also show that cells treated with quinoxalineurea 7c results in caspase 3/7 activation, PARP cleavage and Mcl-1 dependent apoptosis.
authors.affiliation: Eppley Institute for Cancer Research, University of Nebraska Medical Center, Omaha, NE 68198, United States.
authors.forename: Qianyi
authors.initials: Q
authors.lastname: Chen
authors.forename: Vashti C
authors.initials: VC
authors.lastname: Bryant
authors.forename: Hernando
authors.initials: H
authors.lastname: Lopez
authors.forename: David L
authors.initials: DL
authors.lastname: Kelly
authors.forename: Xu
authors.initials: X
authors.lastname: Luo
authors.forename: Amarnath
authors.initials: A
authors.lastname: Natarajan
mesh_terms: D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D011810:Quinoxalines / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D011810:Quinoxalines